PF-9184
物品单位 |
价格 |
品牌 |
支 |
648 |
TargetMol |
- 发布日期: 2023-02-21
- 更新日期: 2023-06-02
产品详细说明
产地 |
China
|
品牌 |
TargetMol
|
货号 |
T21738
|
用途范围 |
Research Grade
|
纯度 |
>98%%
|
CAS编号 |
1221971-47-6
|
规格 |
1mg
|
是否进口 |
否
|
产品描述
PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), IC50 =16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.
体外活性
PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in rheumatoid arthritis (RASF) in synovial fibroblasts derived from patients and has no apparent cytotoxic effects. PF-9184 (0.015-100 μM) potently blocks mPGES-1 ability to synthesize PGE2 from PGH2, and with no apparent inhibitory effects on COX-2 and prostacyclin synthase in cells. PF-9184 (0.015-100 μM) inhibits PGE2 weakly but has no effect on TXB2 synthesis except at 100 μM in human whole blood and modified blood assays. PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM)[1].
体内活性
PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats[1].
Cas No.
1221971-47-6
分子式
C21H14Cl2N2O4S
分子量
461.32
参考文献
[1]Gabriel M, et, al. Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor. Biochem Pharmacol. 2010 May 15; 79(10): 1445-54.
储存和溶解度
DMSO:10 mg/mL (21.7 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Note
For research use only .